626212-33-7Relevant academic research and scientific papers
Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor
Jiang, Wanlong,Tucci, Fabio C.,Chen, Caroline W.,Arellano, Melissa,Tran, Joe A.,White, Nicole S.,Marinkovic, Dragan,Pontillo, Joseph,Fleck, Beth A.,Wen, Jenny,Saunders, John,Madan, Ajay,Foster, Alan C.,Chen, Chen
, p. 4674 - 4678 (2007/10/03)
A series of 3-arylpropionylpiperazines were synthesized as antagonists of the melanocortin-4 receptor. Their potency was found to be increased by replacing the α-methyl substituent of the initial lead 11 with a larger s-Bu or i-Bu group. Further potency enhancement was observed when a glycine or β-alanine was incorporated onto the benzylamine. Some compounds demonstrated good potency, moderate selectivity, and oral bioavailability.
